| 摘要 |
Isoquinoline derivatives (I) are new. Isoquinoline derivatives of formula (I) and their isomers and salts are new. [Image] n : 1-3; A : NR-CZ-R', CZ-NRR' or NR-CZ-NR'R; Z : O or S; R : H or 1-6C alkyl; R' : 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 3-8C cycloalkyl, (3-8C)cycloalkyl(1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl or heteroaryl(1-6C)alkyl; X : N or NR 1>; R 1>H, 1-6C alkyl, 3-8C cycloalkyl, (3-8C)cycloalkyl(1-6C)alkyl, aryl, aroyl, aryl(1-6C)alkyl, heteroaryl, heteroaroyl or heteroaryl(1-6C)alkyl; R 2>1-6C alkoxy, 3-8C cycloalkoxy or (3-8C)cycloalkyl(1-6C)alkoxy; aryl : phenyl or naphthyl optionally substituted with 1-3 of 1-6C alkyl, 1-6C alkoxy, OH, COOH, alkoxycarbonyl, CHO, NO 2, CN, hydroxymethyl, NH 2, mono- or di(1-6C alkyl)amino or halo; heteroaryl : a 5- to 10-membered mono- or bicyclic group with 1-3 heteroatoms (O, S or N), optionally substituted with 1-3 of 1-6C alkyl, 1-6C alkoxy, OH, COOH, alkoxycarbonyl, CHO, NO 2, CN, hydroxymethyl, NH 2, mono- or di(1-6C alkyl)amino or halo. An independent claim is also included for a process for preparing (I). ACTIVITY : Tranquilizer; Antidepressant; Vasotropic; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Neuroprotective; Nootropic; Antimigraine; Cerebroprotective; Cytostatic; Immunomodulator. In a forced swimming test, oral administration of N-(2-(6-methoxy-4-isoquinolinyl)ethyl)acetamide hydrochloride (2.5 mg/kg) to unspecified animals reduced the immobilization time from 102 seconds (control) to 57 seconds. MECHANISM OF ACTION : Melatonin receptor ligand. |
